EP4320104A4 - REGULATION OF PROTEIN EXPRESSION WITH TMP-PROTAC COMPOUNDS - Google Patents

REGULATION OF PROTEIN EXPRESSION WITH TMP-PROTAC COMPOUNDS

Info

Publication number
EP4320104A4
EP4320104A4 EP22785672.1A EP22785672A EP4320104A4 EP 4320104 A4 EP4320104 A4 EP 4320104A4 EP 22785672 A EP22785672 A EP 22785672A EP 4320104 A4 EP4320104 A4 EP 4320104A4
Authority
EP
European Patent Office
Prior art keywords
tmp
regulation
protein expression
protac compounds
protac
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP22785672.1A
Other languages
German (de)
French (fr)
Other versions
EP4320104A1 (en
Inventor
Mark A. Sellmyer
Iris Kyungmin LEE
Andrew Ruff
Nitika Sharma
Jean M. ETERSQUE
Justin NORTHRUP
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Pennsylvania Penn
Original Assignee
University of Pennsylvania Penn
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by University of Pennsylvania Penn filed Critical University of Pennsylvania Penn
Publication of EP4320104A1 publication Critical patent/EP4320104A1/en
Publication of EP4320104A4 publication Critical patent/EP4320104A4/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/04X-ray contrast preparations
    • A61K49/0433X-ray contrast preparations containing an organic halogenated X-ray contrast-enhancing agent
    • A61K49/0442Polymeric X-ray contrast-enhancing agent comprising a halogenated group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • C07D239/49Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/0004Oxidoreductases (1.)
    • C12N9/0012Oxidoreductases (1.) acting on nitrogen containing compounds as donors (1.4, 1.5, 1.6, 1.7)
    • C12N9/0026Oxidoreductases (1.) acting on nitrogen containing compounds as donors (1.4, 1.5, 1.6, 1.7) acting on CH-NH groups of donors (1.5)
    • C12N9/0028Oxidoreductases (1.) acting on nitrogen containing compounds as donors (1.4, 1.5, 1.6, 1.7) acting on CH-NH groups of donors (1.5) with NAD or NADP as acceptor (1.5.1)
    • C12N9/003Dihydrofolate reductase [DHFR] (1.5.1.3)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y105/00Oxidoreductases acting on the CH-NH group of donors (1.5)
    • C12Y105/01Oxidoreductases acting on the CH-NH group of donors (1.5) with NAD+ or NADP+ as acceptor (1.5.1)
    • C12Y105/01003Dihydrofolate reductase (1.5.1.3)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Peptides Or Proteins (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
EP22785672.1A 2021-04-09 2022-04-11 REGULATION OF PROTEIN EXPRESSION WITH TMP-PROTAC COMPOUNDS Pending EP4320104A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202163173087P 2021-04-09 2021-04-09
PCT/US2022/071660 WO2022217295A1 (en) 2021-04-09 2022-04-11 Control of protein expression with tmp-protac compounds

Publications (2)

Publication Number Publication Date
EP4320104A1 EP4320104A1 (en) 2024-02-14
EP4320104A4 true EP4320104A4 (en) 2025-06-04

Family

ID=83546647

Family Applications (1)

Application Number Title Priority Date Filing Date
EP22785672.1A Pending EP4320104A4 (en) 2021-04-09 2022-04-11 REGULATION OF PROTEIN EXPRESSION WITH TMP-PROTAC COMPOUNDS

Country Status (3)

Country Link
US (1) US20240226100A1 (en)
EP (1) EP4320104A4 (en)
WO (1) WO2022217295A1 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012003281A2 (en) * 2010-06-30 2012-01-05 Brandeis University Small-molecule-targeted protein degradation
WO2020041387A1 (en) * 2018-08-20 2020-02-27 The Brigham And Women's Hospital, Inc. Degradation domain modifications for spatio-temporal control of rna-guided nucleases

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES428624A1 (en) * 1974-07-24 1977-01-01 Reyba S A Procedure for the preparation of pyrimidine derivatives. (Machine-translation by Google Translate, not legally binding)
US4438267A (en) * 1980-11-11 1984-03-20 Daluge Susan M Monoheteroring compounds and their use
US20160022642A1 (en) * 2014-07-25 2016-01-28 Yale University Compounds Useful for Promoting Protein Degradation and Methods Using Same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012003281A2 (en) * 2010-06-30 2012-01-05 Brandeis University Small-molecule-targeted protein degradation
WO2020041387A1 (en) * 2018-08-20 2020-02-27 The Brigham And Women's Hospital, Inc. Degradation domain modifications for spatio-temporal control of rna-guided nucleases

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
See also references of WO2022217295A1 *
YANG WANG ET AL: "Degradation of proteins by PROTACs and other strategies", ACTA PHARMACEUTICA SINICA B, vol. 10, no. 2, 1 February 2020 (2020-02-01), pages 207 - 238, XP055767849, ISSN: 2211-3835, DOI: 10.1016/j.apsb.2019.08.001 *

Also Published As

Publication number Publication date
US20240226100A1 (en) 2024-07-11
WO2022217295A1 (en) 2022-10-13
EP4320104A1 (en) 2024-02-14

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Ipc: A61K 31/505 20060101ALI20250205BHEP

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Ipc: A61K 31/45 20060101ALI20250205BHEP

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Ipc: A61K 31/45 20060101ALI20250429BHEP

Ipc: A61K 31/44 20060101ALI20250429BHEP

Ipc: A61K 31/445 20060101ALI20250429BHEP

Ipc: C07D 401/14 20060101ALI20250429BHEP

Ipc: C07D 239/49 20060101AFI20250429BHEP